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    • 1. 发明授权
    • 2-amino-9-alkylpurines: GABA brain receptor ligands
    • 2-氨基-9-烷基嘌呤:GABA脑受体配体
    • US06414147B1
    • 2002-07-02
    • US09470940
    • 1999-12-22
    • Kevin S. CurriePamela AlbaughPaul Chen
    • Kevin S. CurriePamela AlbaughPaul Chen
    • C07D47318
    • C07D473/00C07D473/18C07D473/24
    • Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: W is oxygen or sulfur; X is (un)substituted lower alkyl; or X is (un)substituted aryl or heteroaryl; Y is hydrogen or lower alkyl; Z is lower alkenyl, lower alkynyl, or (un)substituted lower alkyl; T is (un)substituted aryl or heteroaryl. The compounds are highly selective agonists, antagonists, or inverse agonists for GABAa brain receptors, or prodrugs of agonists, antagonists, or inverse agonists for GABAa brain receptors. Thus these compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, Down's Syndrome, overdose with benzodiazepine drugs, and for the enhancement of memory.
    • 公开了下式的化合物或其药学上可接受的无毒盐,其中:W是氧或硫; X是(un)取代的低级烷基; 或者X是(未)取代的芳基或杂芳基; Y是氢或低级烷基; Z是低级烯基,低级炔基或(未)取代的低级烷基; T是(未)取代的芳基或杂芳基。该化合物是高度选择性的激动剂, 拮抗剂或GA​​BAa脑受体的反向激动剂,或GABAa脑受体的激动剂,拮抗剂或反向激动剂的前药。 因此,这些化合物可用于诊断和治疗焦虑症,睡眠和癫痫发作障碍,唐氏综合症,苯并二氮卓类药物过量以及增强记忆功能。